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Details for Patent: 5,650,386

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Details for Patent: 5,650,386

Title: Compositions for oral delivery of active agents
Abstract:Modified amino acid compounds useful for the delivery of active agents are provided. The amino acids, non-alpha-amino acids, have been modified by acylation on the amino group particularly with phenyl or cyclohexyl groups. These groups have a variety of substituents including but not limited to hydroxy, methyl, fluoro, chloro, and the like. The compounds of the invention can be combined with numerous active agents including but not limited to heparin, peptides, and parathyroid hormone, and can then be used for effective administration of the active agent. Administration can be, for example, oral or parenteral.
Inventor(s): Leone-Bay; Andrea (Ridgefield, CT), Ho; Koc-Kan (Mt. Kisco, NY), Press; Jeffery Bruce (Brewster, NY)
Assignee: Emisphere Technologies, Inc. (Hawthorne, NY)
Filing Date:Mar 31, 1995
Application Number:08/414,654
Claims:1. The compound ##STR11## or a salt thereof.

2. A poly amino acid comprising the amino acid ##STR12## or a salt thereof.

3. A poly amino acid as defined in claim 2, comprising a peptide.

4. A composition comprising

(a) an active agent; and

(b) the compound ##STR13## or a salt thereof.

5. A composition comprising

(a) an active agent; and

(b) a poly amino acid comprising the amino acid ##STR14## or a salt thereof.

6. A composition as defined in claim 5, wherein said poly amino acid comprises a peptide.

7. A composition as defined in claim 4, wherein said active agent is selected from the group consisting of a biologically active agent and a chemically active agent.

8. A composition as defined in claim 5, wherein said active agent is selected from the group consisting of a biologically active agent and a chemically active agent.

9. A composition as defined in claim 7, wherein said biologically active agent is selected from the group consisting of a peptide, a mucopolysaccharide, a carbohydrate, a lipid, a pesticide, and any combination thereof.

10. A composition as defined in claim 8, wherein said biologically active agent is selected from the group consisting of a peptide, a mucopolysaccharide, a carbohydrate, a lipid, a pesticide, and any combination thereof.

11. A composition as defined in claim 9, wherein said biologically active agent is selected from the group consisting of human growth hormone, bovine growth hormone, growth hormone-releasing hormone, an interferon, interleukin-II, insulin, heparin, calcitonin, erythropoietin, atrial naturetic factor, an antigen, a monoclonal antibody, somatostatin, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, vasopressin, cromolyn sodium, vancomycin, desferrioxamine (DFO), and any combination thereof.

12. A composition as defined in claim 10, wherein said biologically active agent is selected from the group consisting of human growth hormone, bovine growth hormone, growth hormone-releasing hormone, an interferon, interleukin-II, insulin, heparin, calcitonin, erythropoietin, atrial naturetic factor, an antigen, a monoclonal antibody, somatostatin, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, vasopressin, cromolyn sodium, vancomycin, desferrioxamine (DFO), and any combination thereof.

13. A composition as defined in claim 4, wherein said active agent comprises a polysaccharide.

14. A composition as defined in claim 5, wherein said active agent comprises a polysaccharide.

15. A composition as defined in claim 13, wherein said active agent comprises a mixture of mucopolysaccharides.

16. A composition as defined in claim 14, wherein said active agent comprises a mixture of mucopolysaccharides.

17. A composition as defined in claim 15, wherein said mixture of mucopolysaccharides comprises heparin.

18. A composition as defined in claim 16, wherein said mixture of mucopolysaccharides comprises heparin.

19. A composition as defined in claim 17, wherein said heparin comprises low molecular weight heparin.

20. A composition as defined in claim 18, wherein said heparin comprises low molecular weight heparin.

21. A composition as defined in claim 11, wherein said biologically active agent comprises human growth hormone.

22. A composition as defined in claim 12, wherein said biologically active agent comprises human growth hormone.

23. A dosage unit form comprising

(A) a composition as defined in claim 4; and

(B)

(a) an excipient,

(b) a diluent,

(c) a disintegrant,

(d) a lubricant,

(e) a plasticizer,

(f) a colorant,

(g) a dosing vehicle, or

(h) any combination thereof.

24. A dosage unit form comprising

(A) a composition as defined in claim 5; and

(B)

(a) an excipient,

(b) a diluent,

(c) a disintegrant,

(d) a lubricant,

(e) a plasticizer,

(f) a colorant,

(g) a dosing vehicle, or

(h) any combination thereof.

25. A dosage unit form according to claim 23, comprising a tablet, a capsule, or a liquid.

26. A dosage unit form according to claim 24, comprising a tablet, a capsule, or a liquid.

27. A composition as defined in claim 24, wherein said poly amino acid comprises a peptide.

28. A composition as defined in claim 23, wherein said active agent is selected from the group consisting of a biologically active agent and a chemically active agent.

29. A composition as defined in claim 24, wherein said active agent is selected from the group consisting of a biologically active agent and a chemically active agent.

30. A composition as defined in claim 28, wherein said biologically active agent is selected from the group consisting of a peptide, a mucopolysaccharide, a carbohydrate, a lipid, a pesticide, and any combination thereof.

31. A composition as defined in claim 29, wherein said biologically active agent is selected from the group consisting of a peptide, a mucopolysaccharide, a carbohydrate, a lipid, a pesticide, and any combination thereof.

32. A composition as defined in claim 30, wherein said biologically active agent is selected from the group consisting of human growth hormone, bovine growth hormone, growth hormone-releasing hormone, an interferon, interleukin-II, insulin, heparin, calcitonin, erythropoietin, atrial naturetic factor, an antigen, a monoclonal antibody, somatostatin, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, vasopressin, cromolyn sodium, vancomycin, desferrioxamine (DFO), and any combination thereof.

33. A composition as defined in claim 31, wherein said biologically active agent is selected from the group consisting of human growth hormone, bovine growth hormone, growth hormone-releasing hormone, an interferon, interleukin-II, insulin, heparin, calcitonin, erythropoietin, atrial naturetic factor, an antigen, a monoclonal antibody, somatostatin, adrenocorticotropin, gonadotropin releasing hormone, oxytocin, vasopressin, cromolyn sodium, vancomycin, desferrioxamine (DFO), and any combination thereof.

34. A composition as defined in claim 23, wherein said active agent comprises a polysaccharide.

35. A composition as defined in claim 24, wherein said active agent comprises a polysaccharide.

36. A composition as defined in claim 34, wherein said active agent comprises a mixture of mucopolysaccharides.

37. A composition as defined in claim 35, wherein said active agent comprises a mixture of mucopolysaccharides.

38. A composition as defined in claim 36, wherein said mixture of mucopolysaccharides comprises heparin.

39. A composition as defined in claim 37, wherein said mixture of mucopolysaccharides comprises heparin.

40. A composition as defined in claim 38, wherein said heparin comprises low molecular weight heparin.

41. A composition as defined in claim 39, wherein said heparin comprises low molecular weight heparin.

42. A composition as defined in claim 32, wherein said biologically active agent comprises human growth hormone.

43. A composition as defined in claim 33, wherein said biologically active agent comprises human growth hormone.

44. A method for preparing a composition, said method comprising mixing:

a) at least one biologically active agent;

b) at least one compound as defined in claim 1; and

c) optionally a dosing vehicle.

45. A method for preparing a composition, said method comprising mixing:

a) at least one biologically active agent;

b) at least one poly amino acid as defined in claim 2; and

c) optionally a dosing vehicle.

46. A method as defined in claim 45, wherein said poly amino acid comprises a peptide.

47. A method as defined in claim 44, wherein said biologically active agent comprises human growth hormone.

48. A method as defined in claim 45, wherein said biologically active agent comprises human growth hormone.

49. A method as defined in claim 44, wherein said biologically active agent comprises polysaccharide.

50. A method as defined in claim 45, wherein said biologically active agent comprises polysaccharide.

51. A method as defined in claim 49, wherein said polysaccharide comprises a mixture of muco-polysaccharides.

52. A method as defined in claim 50, wherein said polysaccharide comprises a mixture of muco-polysaccharides.

53. A method as defined in claim 51, wherein said mixture of muco-polysaccharides comprises heparin.

54. A method as defined in claim 52, wherein said mixture of muco-polysaccharides comprises heparin.

55. A method as defined in claim 53, wherein said heparin comprises low molecular weight heparin.

56. A method as defined in claim 54, wherein said heparin comprises low molecular weight heparin.

57. A method for administering a biologically-active agent to an animal in need of said agent, said method comprising administering orally to said animal a composition as defined in claim 4.

58. A method for administering a biologically-active agent to an animal in need of said agent, said method comprising administering orally to said animal a composition as defined in claim 5.

59. A method for administering a biologically-active agent to an animal in need of said agent, said method comprising administering orally to said animal a composition as defined in claim 15.

60. A method for administering a biologically-active agent to an animal in need of said agent, said method comprising administering orally to said animal a composition as defined in claim 16.

61. A method for administering a biologically-active agent to an animal in need of said agent, said method comprising administering orally to said animal a composition as defined in claim 17.

62. A method for administering a biologically-active agent to an animal in need of said agent, said method comprising administering orally to said animal a composition as defined in claim 18.

63. A method for administering a biologically-active agent to an animal in need of said agent, said method comprising administering orally to said animal a composition as defined in claim 19.

64. A method for administering a biologically-active agent to an animal in need of said agent, said method comprising administering orally to said animal a composition as defined in claim 20.

65. A method for administering a biologically-active agent to an animal in need of said agent, said method comprising administering orally to said animal a composition as defined in claim 21.

66. A method for administering a biologically-active agent to an animal in need of said agent, said method comprising administering orally to said animal a composition as defined in claim 22.
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